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Assay Detail

CHEMBL4179920

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of sodium channel site2 (unknown origin) by radioligand binding assay relative to control
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes.
Storer RI, Pike A, Swain NA, Alexandrou AJ, Bechle BM, Blakemore DC, Brown AD, Castle NA, Corbett MS, Flanagan NJ, Fengas D, Johnson MS, Jones LH, Marron BE, Payne CE, Printzenhoff D, Rawson DJ, Rose CR, Ryckmans T, Sun J, Theile JW, Torella R, Tseng E, Warmus JS.
Bioorg Med Chem Lett (2017) 27 : 4805 -4811
PubMed 29029933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.32 7.32
Ki 1 7.37 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217988 2 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217988 Ki = 43.0 nM 7.37
CHEMBL4217988 IC50 = 48.0 nM 7.32